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Re: Sublingual GABA and nicotinamide?

Posted by Paulie on May 30, 2003, at 18:12:22

In reply to Sublingual GABA and nicotinamide?, posted by btnd on May 30, 2003, at 14:19:38

Very good question. Unfortunately the answer is probably no. GABA does not cross the BBB(blood-brain barrier) very easily. It has low permeability with respect to BBB and only a small % actually makes it across. Taking it as a sublingual does not change that fact. Picamilon(nicotinyl-y-aminobutyric acid) on the other hand rapidly crosses the BBB. It was developed in Russia and has both tranquilizing and stimulating properties. Picamilon is actually Niacin (not nicotinamide-same as niacinamide) bonded to GABA.

How And Why Picamilon Works
by R. P. Kruglikova

Drugs that normalize the gamma aminobutyric acid (GABA) system consist mainly of substances that activate GABA receptors, inhibit GABA utilization or increase the permeability of the blood-brain barrier to GABA. One-way of creating preparations of this kind is to use substances that are carriers of the GABA molecule, including vitamins or their derivatives and, in particular, nicotinic acid (niacin).

Niacin has been chosen as the carrier because of its valuable pharmacological properties, its low toxicity, and its high biological availability. It has therefore been suggested that a combination of niacin and GABA in the same molecule would increase the potency of each component.
Picamilon (nicotinyl-y-aminobutyric acid) was first synthesized at the All-Union Vitamin Research Institute in 1970. It is a white crystalline powder that is odorless, highly hygroscopic (takes up moisture readily), and readily soluble in water.

In studies in animals Picamilon has been shown to have positive action on the cerebral circulation, and also exhibits the properties of a tranquilizer with a stimulating component. Unlike tranquilizer drugs, Picamilon does not induce muscle relaxation, drowsiness or lethargy.

For more info:
http://www.smart-drugs.com/picamilon-article.htm


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